Directions for Use

PD184352 is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 5 mg in 1044.6 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-10 µM for 0.5-1 hr prior to treating with a stimulator or is used alone with varying treatment times lasting up to 24 hr. Soluble in DMSO at 25 mg/ml and ethanol at 8 mg/ml with warming; poorly soluble in water with maximum solubility in water at ~5-10 µM.

Background

PD184352 (CI-1040) is a highly potent and selective noncompetitive MEK inhibitor with an IC50 of 17 nM for MEK1 (1). Treatment of cells with PD184352 leads to suppression of MAPK activation (1-4) and potently inhibits the proliferation of cells harboring the B-Raf mutation V600E (2,3). Researchers have shown that PD184352 effectively inhibits MEK5, although not as potently as MEK1 (4).